KRN2 bromide

Research use only, not for human use.

KRN2 bromide is a selective NFAT5 inhibitor with an IC50 of 100 nM.?

KRN2 bromide is a selective NFAT5 inhibitor with an IC50 of 100 nM.?(In Vitro):KRN2 bromide inhibits the NF-κB p65 binding to Nfat5 promoter 1 in a dose-dependent manner and directly blocks the interaction between NF-κB p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1) of Nfat5 exon 1. KRN2 bromide selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions.(In Vivo):In DBA/1J mice immunized with bovine type II collagen, KRN2 bromide (3 mg/kg, i.p.) effectively suppresses CIA as well as AIA in which innate immune cells play a predominant role, and decreases the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.

KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions.KRN2 dose-dependently inhibits the NF-κB p65 binding to Nfat5 promoter 1 and directly blocks the interaction between NF-κB p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1) of Nfat5 exon 1.

KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play a predominant role.KRN2 (3 mg/kg, i.p., daily) effectively suppresses CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration. Animal Model:8-week-old C57BL/6 mice injected intradermally with 2 mg of complete Freund's adjuvant.Dosage:3 mg/kg.Administration:Peritoneally (i.p.) daily for 2 weeks.Result:Effective in suppressing AIA.Animal Model:8-week-old DBA/1J mice immunized with bovine type II collagen.Dosage:3 mg/kg.Administration:Peritoneally (i.p.) daily.Result:Effective in suppressing CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.

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Others

Other Targets

Caspase-3

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1390654-28-0

524.386

C27H23BrFNO4

>98% (HPLC)

In Vitro:?DMSO : 18.33 mg/mL (34.96 mM)

[Br-].COc1ccc2c(Cc3ccccc3F)c3-c4cc5OCOc5cc4CC[n+]3cc2c1OC

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(-20℃)

With Ice Pack

≥ 2 years